FLUOCINONIDE 2.5MG CREAM

Indications

• Eczema
• Psoriasis
• Chronic localized recalcitrant dermatoses
• Severe inflammatory skin disorders unresponsive to less potent corticosteroids

Dosage

Children: Children aged 1–17 years: Apply thinly to the affected area 1–2 times daily, reducing strength as the condition responds.

Adults: Apply thinly to the affected area 1–2 times daily. Strength may be reduced as the condition improves.

Mechanism of action

Fluocinonide binds to the cytosolic glucocorticoid receptor, forming a receptor-ligand complex that translocates into the cell nucleus. There, it binds to glucocorticoid response elements (GRE) in the promoter region of target genes, leading to the increased expression of specific genes. The anti-inflammatory effects are mediated through the induction of lipocortins, which inhibit phospholipase A2 and subsequently decrease the production of eicosanoids, including prostaglandins and leukotrienes. This action also suppresses cyclooxygenase expression, further enhancing anti-inflammatory effects.

Pharmacodynamics

As a potent glucocorticoid, fluocinonide mediates anti-inflammatory actions that relieve the signs and symptoms of inflammatory skin conditions. It effectively reduces itching, redness, dryness, and scaling, thereby improving overall skin comfort and appearance.

Pharmacokinetics

Fluocinonide is applied topically, and its systemic absorption varies based on the site of application, the formulation used, and the condition of the skin. It is metabolized in the liver, and its metabolites are excreted primarily via the urine. The onset of action can occur within hours of application, with a duration of effect that can last for several days depending on the condition treated and the formulation used.

Adverse effects

• Cushing's syndrome
• Increased risk of infection
• Vasodilation

Precautions

• Patients or carers should be counselled on the application of fludroxycortide cream and ointment.

Pregnancy

Use with caution. The effects on pregnancy are not well established, and benefits should outweigh the risks.

Breast-feeding

Use with caution. Limited data is available on the excretion of fluocinonide in breast milk.

Storage

Store in a cool, dry place away from direct sunlight. Keep out of reach of children.

Formulations

• 0.025% cream
• 0.05% cream
• 0.0125% ointment
• 0.025% gel

Mechanism of action

Fluocinonide is a potent glucocorticoid steroid used topically as anti-inflammatory agent for the treatment of skin disorders such as eczema. Fluocinonide binds to the cytosolic glucocorticoid receptor. After binding the receptor the newly formed receptor-ligand complex translocates itself into the cell nucleus, where it binds to many glucocorticoid response elements (GRE) in the promoter region of the target genes. The DNA bound receptor then interacts with basic transcription factors, causing the increase in expression of specific target genes. The anti-inflammatory actions of corticosteroids are thought to involve lipocortins, phospholipase A2 inhibitory proteins which, through inhibition arachidonic acid, control the biosynthesis of prostaglandins and leukotrienes. Specifically glucocorticoids induce lipocortin-1 (annexin-1) synthesis, which then binds to cell membranes preventing the phospholipase A2 from coming into contact with its substrate arachidonic acid. This leads to diminished eicosanoid production. Cyclooxygenase (both COX-1 and COX-2) expression is also suppressed, potentiating the effect. In another words, the two main products in inflammation Prostaglandins and Leukotrienes are inhibited by the action of Glucocorticoids. Glucocorticoids also stimulate the lipocortin-1 escaping to the extracellular space, where it binds to the leukocyte membrane receptors and inhibits various inflammatory events: epithelial adhesion, emigration, chemotaxis, phagocytosis, respiratory burst and the release of various inflammatory mediators (lysosomal enzymes, cytokines, tissue plasminogen activator, chemokines etc.) from neutrophils, macrophages and mastocytes. Additionally the immune system is suppressed by corticosteroids due to a decrease in the function of the lymphatic system, a reduction in immunoglobulin and complement concentrations, the precipitation of lymphocytopenia, and interference with antigen-antibody binding. Like other glucocorticoid agents Fluocinolone acetonide acts as a physiological antagonist to insulin by decreasing glycogenesis (formation of glycogen). It also promotes the breakdown of lipids (lipolysis), and proteins, leading to the mobilization of extrahepatic amino acids and ketone bodies. This leads to increased circulating glucose concentrations (in the blood). There is also decreased glycogen formation in the liver.

Pharmacodynamics

Fluocinonide is a potent glucocorticoid steroid used topically as anti-inflammatory agent for the treatment of skin disorders such as eczema. It mediates its effects to relieve itching, redness, dryness, crusting, scaling, inflammation, and discomfort associated with inflammatory skin conditions.